| 摘要 |
Disclosed is a compound of formula I or pharmaceutically acceptable prodrugs, salts, hydrates, solvates, crystal forms or diastereomers thereof, wherein: R1 is H, C1-6alkyl, C1-6alkylNR5R6, C1-6alkylNR5COR6, C1-6alkylNR5SO2R6, C1-6alkylCO2R5, C1-6alkylCONR5R6, where R5 and R6 are each independently H, C1-4alkyl, aryl, hetaryl, C1-4alkylaryl, C1-4alkylhetaryl or may be joined to form an optionally substituted 3-8 membered ring optionally containing an atom selected from O, S, NR7 and R7 is selected from H, C1-4alkyl; R2, R3 and R4 are each independently H, halogen, C1-4alkyl, OH, OC1-4alkyl, CF3, OCF3, CN, C1-4alkylNR8R9, OC1-4alkylNR8R9, OCONR8R9, NR8R9, NR8COR9, NR10CONR8R9, NR8SO2R9, COOR8, CONR8R9; and R8, R9 are each independently H, C1-4alkyl, C1-4alkyl cycloalkyl, or may be joined to form an optionally substituted 3-8 membered ring optionally containing an atom selected from O, S, NR11; R10 and R11 are independently selected from H, C1-4alkyl, CF3; alternatively, two of R2, R3 and R4, when located on adjacent carbon atoms, may be joined to form a ring system as depicted in the specification; Q is C1-4alkyl; W is selected from C2-4alkyl, C2-6alkenyl; where C2-4alkyl or C2-6alkenyl may be optionally substituted with C1-4alkyl, OH, OC1-4alkyl, NR15R16; and R15, and R16 are each independently H, C1-4alkyl, C1-4alkyl cycloalkyl, C1-4alkyl cyclohetalkyl, aryl, hetaryl, or may be joined to form an optionally substituted 3-8 membered ring optionally containing an atom selected from O, S, NR17 and R17 is selected from H, C1-4alkyl; A is aryl, hetaryl optionally substituted with 0-3 substituents independently chosen from halogen, C1-4alkyl, CF3, aryl, hetaryl, OCF3, OC1-4alkyl, OC2-5alkylNR18R19, Oaryl, Ohetaryl, CO2R18, CONR18R19, NR18R19, C1-4alkylNR18R19, NR20C1-4alkylNR18R19, NR18COR19, NR20CONR18R19, NR18SO2R19; and R18, R19 are each independently H, C1-4alkyl, C1-4alkyl cyclohetalkyl, aryl, hetaryl, C1-4alkyl aryl, C1-4alkyl hetaryl, or may be joined to form an optionally substituted 3-8 membered ring optionally containing an atom selected from O, S, NR21; and R20 is selected from H, C1-4alkyl; and R21 is selected from H, C1-4alkyl; and Y is selected from H, C1-4alkyl, OH, NR22R23, and R22, and R23 are each independently H, C1-4alkyl. The compounds may be used to prepare a medicament for the treatment of a hyperproliferation-related disease state. Reference has been directed by the Commissioner under Section 14 to Patent Specification 537155.
|
